scholarly journals Optimization of Self-Micro Emulsifying Drug Delivery System) for Soursop Leaf (Annona muricata Linn.) Chloroform Extract

2020 ◽  
Vol 25 (2) ◽  
pp. 81
Author(s):  
Anif Nur Artanti ◽  
Fea Prihapsara ◽  
Dian Eka Ermawati ◽  
Aprilia Saefanan Shofa
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Statistical Analysis ◽  
Zeta Potential ◽  
Propylene Glycol ◽  
Drug Delivery System ◽  
Delivery System ◽  
Tween 80 ◽  
Chloroform Extract ◽  
T Test

Soursop leaf chloroform extract has anticancer activity.  The active ingredient of soursop leaf was acetogenin polypoid derivatives that have a lipophilic characteristic, and less effective to achieve action targets of drugs in biological systems. The Self-Micro Emulsifying Drug Delivery System (SMEDDS) was an effective drug delivery technique that increases the solubility of lipophilic drugs. This study aims to determine the proportion of optimum SMEDDS formula using Simplex Lattice Design (SLD) method. The Formula of SMEDDS was prepared using a combination of Tween 80-Croduret, Propylene Glycol, and Candlenut oil. Optimization formula with SLD method using Design-Expert software based on physical stability parameters there are the percent of transmittance and emulsification time. The optimum formula of SMEDDS was compared with SLD prediction formula using a statistical analysis t-test, then test of loading dose extract, stability test accelerated by centrifugation, particle size, and zeta potential. The proportion of optimum composition of Tween 80-Croduret, Propylene Glycol, and Candlenut oil of SMEDDS was 60.87%; 24.13%; 15.00% respectively. Results of transmittance 41.14±3.78% and emulsification time 119.0±2.08 seconds. The predicted SLD value for the transmittance percent was 55.0% and the emulsification time was 119.59 seconds. The result of the statistical analysis of one sample t-test showed no significant difference between observation results and SLD prediction. The SMEDDS system has F value of 0.99 and capable to load 25.0 mg chloroform extract of soursop leaf each system with an average particle size of 440 nm and zeta potential of +21.5 mV. 

scholarly journals OPTIMIZATION AND CHARACTERIZATION OF FORMULATION SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM ETHANOL EXTRACT OF ROMANG PARANG LEAVES (BOEHMERIA VIRGATA)

2021 ◽  
pp. 207-212
Author(s):  
MAGFIRAH ◽  
INDAH KURNIA UTAMI
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Secondary Metabolites ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Loading ◽  
Ethanol Extract ◽  
Polydispersity Index ◽  
Lattice Design

Objective: Parang romang (Boehmeria virgata) is one of the traditional medicines that are used empirically by Makassar tribal healers, South Sulawesi, as an antitumor drug. This traditional medicine contains secondary metabolites such as alkaloids, flavonoids, tannins, and saponins. However, secondary metabolites of those leaves extract have low solubility in water. Hence, to be formula, self-nanoemulsifying drug delivery system (SNEDDS) is one of the solutions to increase the extract solubility. Methods: The optimization of two formula optimum SNEDDS parang romang leaves (T80PGMZ and T20PGMZ) was using the simple lattice design (SLD) method which will give 28 SNEDDS formula parang romang leaves each of which the formula is tested for its characteristics as a critical point include emulsification time, % transmittance, drug loading, particle size, zeta potential, polydispersity index, and morphology particle. Results: The results of SNEDDS characterization obtained the optimum formula T80PGMZ with emulsification time 12.6 s, % transmittance 92.21%, drug loading 68.21 ppm, particle size 370.26 nm, zeta potential −31.4 mV, polydispersity index of 0.615, and regular particle morphology with spherical chunks at a magnification of 10,000 times with a particle size of 10 μm. Conclusion: SNEDDS of parang romang leaves extracts that used olive oil as oil phase, Tween 80 as a surfactant, and propylene glycol as the cosurfactant provided nanoemulsion with good characteristics.

scholarly journals PHYSICOCHEMICAL CHARACTERIZATION OF PROPRANOLOL-LOADED CHITOSAN NANOPARTICLES FOR A BUCCAL DRUG DELIVERY SYSTEM

2020 ◽  
pp. 243-247
Author(s):  
SIRIPORN KITTIWISUT ◽  
PAKORN KRAISIT
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Chitosan Nanoparticles ◽  
Particle Sizes ◽  
Zeta Potentials ◽  
Ph Values ◽  
Buccal Drug Delivery

Objective: This study aimed to characterize the physicochemical properties, including pH, zeta potential, and particle size of propranolol-loaded nanoparticles that were incorporated into a buccal transmucosal drug-delivery system. Methods: An ionotropic gelation technique was used to formulate propranolol-loaded chitosan nanoparticles. Chitosan used as the nanoparticle base, using tripolyphosphate (TPP) as a cross-linking agent. The effects on nanoparticle physical properties, including pH, zeta potential, and particle size were examined when various chitosan [0.150-0.300 % (w/v)] and propranolol contents (0-40 mg) were used during the preparation. The effects of using chitosan solutions with different pH values on nanoparticle properties were also determined. Results: The pH values of all nanoparticles ranged between 4.14–4.55. The zeta potentials of the prepared nanoparticles ranged between 22.6–52.6 mV, with positive charges. The nanoparticle sizes ranged from 107–140 nm, which are within the range of suitable particle sizes for transmucosal preparations. Conclusion: The pH values, zeta potentials, and particle sizes of the nanoparticle formulations were influenced by the concentrations of chitosan and propranolol and by the pH of the initial chitosan solution. The relationships between nanoparticle properties and all factors primarily depended on the ionic charges of the components, especially chitosan. Our study provides beneficial physicochemical knowledge for the further development of chitosan-based nanoparticles containing propranolol for buccal drug delivery systems.

scholarly journals Vegetable Oil-Based Self-Microemulsifying Drug Delivery System of Eprosartan Mesylate: in vitro and ex vivo Evaluation

2021 ◽  
Vol 33 (9) ◽  
pp. 2182-2190
Author(s):  
Sabitri Bindhani ◽  
Snehamayee Mohapatra ◽  
Rajat Kumar Kar
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Delivery System ◽  
Intestinal Permeability ◽  
Delivery System ◽  
Ex Vivo ◽  
Tween 80 ◽  
Stability Study ◽  
Potent Drug

This study was planned to increase the intestinal permeability and thereby bioavailability of eprosartan mesylate (EPM) by designing a self-microemulsifying drug delivery system (SMEDDS) by the use of vegetable oils. Various SMEDDS-based formulations were prepared with oleic acid and peppermint oil. Tween 80 was used as surfactant and PEG 400 as co-surfactant. Pseudo ternary phase diagrams were constructed for identifying emulsification region between 1:1, 1:2, 2:1, 3:1 ratio of SCOS mix. Eight batches of SMEDDS were found to be thermodynamically stable and from which SMEDDSOF9 and PF5 were best formulations due to their highest drug content, minimum particle size. They have shown highest release of drug in vitro and higher in vitro drug diffusion and ex vivo permeation analysis than pure drug. FTIR study ascertained no incompatibility between drug and excipients present in formulation. From the accelerated stability study, slight effect on particle size and zeta potential, assay content along with cumulative % of drug release was found. The results demonstrated the SMEDDS of EPM are potent drug delivery system to increase dissolution rate and bioavailability of drug via increased intestinal permeability and consequently improving the therapeutic efficacy of eprosartan mesylate.

scholarly journals Formulation and Evaluation of Herbal Drug Loaded Self Nano Emulsifying Drug Delivery System (SNEDDS)

2018 ◽  
Vol 3 (2) ◽  
pp. 26-36
Author(s):  
Vishal N Kushare ◽  
Saravanan S
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Tween 80 ◽  
Water Soluble ◽  
Coriandrum Sativum ◽  
Polydispersity Index ◽  
Drug Dissolution ◽  
Reduced Pressure

The goal of this research was to formulate and test invitro the self-nano emulsifying drug delivery system (SNEDDS) of poorly water-soluble herbal material. Linalool, an essential of Coriandrum sativum with anti-epileptic activity, was isolated from Coriandrum sativum by using Soxhlet extraction method followed by column chromatography and fractionates are concentrated under reduced pressure by using rotary flash evaporator. It is low water soluble material; unpredictable dissolution and low bioavailability make it very difficult to administer linalool orally.The captex-200 oil was exhibited maximum solubility of linalool. Thus, it was chosen as the oil phase, while Tween 80 and PEG-200 were chosen as surfactant and co-surfactant respectively for the preparation of linalool SNEDDS. For the determination of existence zone of nanoemulsion, pseudo ternary phase diagram was developed using the Prism Software by using water titration method. Self-nanoemulsion are evaluated for scanning electron microscopy (SEM), particle size analysis, polydispersity index, zeta potential and invitro drug release.The s9 formulation showed 97.72% cumulative release higher than other selected formulations(S4-S8). The S9 formulation showed promising result on droplet size, zeta potential, polydispersity index, invitro drug dissolution. It was concluded that SNEDDS formation from captex-200, tween 80, PEG-200, Smix (4:1), is a promising approach to enhancing substance solubility and the pace of dissolution.

scholarly journals Novel combination for Self-nanoemulsifying Drug Delivery System of Candesartan Cilexetil

2018 ◽  
pp. 123-134
Author(s):  
Safa Fakher Mekhilef ◽  
Ahmed A. Hussein
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Water Solubility ◽  
Candesartan Cilexetil ◽  
Promising Result ◽  
Potential Measurement

Solubility problem of many of effective pharmaceutical molecules are still one of the major obstacle in theformulation of such molecules. Candesartan cilexetil (CC) is angiotensin II receptor antagonist with very low water solubility and this result in low and variable bioavailability. Self- emulsifying drug delivery system (SEDDS) showed promising result in overcoming solubility problem of many drug molecules. CC was prepared as SEDDS by using novel combination of two surfactants (tween 80 and cremophore EL) and tetraglycol as cosurfactant, in addition to the use of triacetin as oil. Different tests were performed in order to confirm the stability of the final product which includes thermodynamic study, determination of self-emulsification time, particle size and zeta potential measurement, and in-vitro drug release. The results showed that the particle size of the best formula was 13.3 nm and zeta potential of -37.45 mV with approximately 100% release after 45 minutes .These results suggest that the preparation of CC. as SEDDS with the use of the above combination of surfactant and cosurfactant is a promising maneuver for oral delivery of CC. in order to improve its bioavailability.   

Enhancement of Nimodipine Solubility by Self-Nano-emulsifying Drug Delivery System

2019 ◽  
Vol 12 (5) ◽  
pp. 4648-4656
Author(s):  
Suresh Gande ◽  
S. Srikanth Reddy ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Spherical Shape ◽  
Drug Dissolution ◽  
The Stability

Self-nanoemulsifying drug delivery system (SNEDDS) of Nimodipine was developed with the purpose of improving the bioavailability of the drug. Based on the results of Nimodipine solubility studies Peceol, Transcutol P and PEG 400 were optimized as oil, surfactant and co-surfactant for the formulation and Pseudo ternary plots was constructed by Chemix software. Fifteen formulations of Nimodipine SNEDDS prepared and analyzed for particle size, emulsification time, percentage drug release, percentage transmittance, in vitro drug dissolution studies and thermodynamic stability. The optimized Nimodipine SNEDDS formulation (F13) subjected to drug-excipient compatibility studies by FTIR. They are analyzed for zeta potential, SEM and stability. The particle size of optimized Nimodipine SNEDDS formulation was 25.9 nm, PDI is 0.382 and zeta potential -12.7 mV that are optimal for the stability of emulsion. SEM studies of Nimodipine SNEDDS indicated spherical shape and uniform particle distribution. The drug release of formulation F13 (98.25±4.77%) was higher than pure drug (38.49±3.88%). The stability studies indicated no change in drug content, drug release, emulsifying properties and appearance. Hence a potential SNEDDS formulation of Nimodipine developed with increased dissolution rate, bioavailability and solubility.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF SUSTAINED RELEASE METHOTREXATE LOADED CUBOSOMES FOR TOPICAL DELIVERY IN RHEUMATOID ARTHRITIS

2020 ◽  
pp. 33-39
Author(s):  
KARISHMA KAPOOR ◽  
VINAY PANDIT ◽  
UPENDRA NAGAICH
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Poloxamer 407

Objective: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are essential part of the administration of Rheumatoid Arthritis (RA). Methotrexate (MTX) is effective for tumor necrosis factor alpha (TNF-a) biologic agents, indicated only in minority of patients suffering from severe RA. MTX remains the "anchor drug" in the treatment of RA. For delivery improvement, novel pharmaceutical drug delivery system i.e. MTX-Cubosomes were developed. Methods: Poloxamer 407 and Glycerol monooleate (Monoelin, MO) used and the formulation were characterized as a sustained release drug delivery system for Methotrexate. Different ratios of Monolein, Poloxamer 407 and water were used to develop the different cubosomes using homogenization and emulsification method. Characterization of formulations for morphology was performed and also particle size distribution by Transmission Electron Microscopy (TEM). Results: Formulation showed the internal cubic structures of the vesicles. The particle size of the formulations was found to be ranging from 53.21 to 185.32 nm, zeta potential of the formulations varied from-18.20-36.10 mV. The cubosomal formulation exhibited good entrapment efficiency along with high drug loading. Compatibility with the excipients was also established. An in vitro release study was done using Franz Diffusion cell indicated sustained release of the formulation at a rate of 1.25 %/h. Cubosomes proved to be reliable system for sustained transdermal drug delivery system. Conclusion: Methotrexate cubosomes is a novel medication delivery framework and in this examination it has been developed and characterized. The formulations were found to be promising in terms of its characterization parameters like particle size, zeta potential, entrapment efficiency, loading capacity, release kinetics, and stability, suitable for topical delivery.

scholarly journals FORMULATION DEVELOPMENT AND IN VITRO ANTIOXIDANT AND ANTIDIABETIC EVALUATION OF ERIOBOTRYA JAPONICA BASED SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM

2019 ◽  
pp. 313-319
Author(s):  
AMRIT PAL SINGH ◽  
GOPAL L. KHATIK ◽  
VIJAY MISHRA ◽  
NAVNEET KHURANA ◽  
NEHA SHARMA ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Droplet Size ◽  
Delivery System ◽  
Methanolic Extract ◽  
Tween 80 ◽  
Eriobotrya Japonica ◽  
Formulation Development

Objective: The aim of the present study was to develop and characterize self-nano emulsifying drug delivery system (SNEDDS) of methanolic extract of Eriobotrya japonica (Thunb.) Lindl. (E. japonica) leaves. Further in vitro antioxidant and antidiabetic potential of an optimized batch of SNEDDS was explored. Methods: Oil (Labrafil M 1944 CS), surfactant (Tween 80) and co-surfactant (Transcutol P) were selected on the basis of solubility of the methanolic extract. Twenty-seven batches of SNEDDS were prepared with different compositions of oil, surfactant and co-surfactant. The optimized batch was evaluated for its entrapment efficiency, droplet size, polydispersity index (PDI), zeta potential, transmission electron microscopy (TEM). Further, DPPH assay and α-amylase activity were also performed to check the antioxidant and antidiabetic potential of prepared SNEDDS. Results: The optimized design suggested that 10% of Labrafil M 1944CS, 30% of Tween 80 and 60% of Transcutol P could develop SNEDDS with 208 nm mean droplet size, 99.64% drug loading, 0.156 PDI and-6 mV zeta potential. TEM image confirmed the droplet size less than 100 nm and the spherical shape of SNEDDS. In vitro antioxidant and antidiabetic activities of SNEDDS revealed the increased efficacy as compared to that of the ascorbic acid and acarbose, respectively. Conclusion: The optimized batch of SNEDDS was found to improve the antioxidant and antidiabetic efficacy of methanolic extract of E. japonica.

scholarly journals Self Nano-Emulsifying Drug Delivery System (SNEDDS) of Curcuma Mangga Val. Essential Oil and The Stability Study

2020 ◽  
pp. 238-243
Author(s):  
Retno Sunarminingsih Sudibyo ◽  
Lukman Mahdi ◽  
Ronny Martien
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Essential Oil ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Droplet Size ◽  
Delivery System ◽  
Stability Study ◽  
Freeze Thaw ◽  
Lattice Design

Essential oil of Curcuma mangga Val. has been reported to have cytotoxic effect against cancer cell lines. But this oil is unstable in dispensing so that a self nano-emulsifying drug delivery system (SNEDDS) of the oil was conducted to solve the problem and improve its potency. In the study, optimization, verification, characterization, and stability test of the SNEDDS formula were carried out respectively by simplex lattice design (SLD) on Design Expert ver. 10 software, droplet size and Zeta potential determinations using particle size analyzer (PSA) instrument, as well as heating-cooling and freeze-thaw methods. The best SNEDDS formula resulted was Miglyol : Tween 80 : PEG 400 = 16.034% : 68.380% : 15.586%; with transmittance of 84.47 + 1.05%, droplet size of 15.75 nm, zeta potential of -8.54 mV, polydispersity index (PDI) of 0.188, emulsifying time of 49.67 + 1.7 seconds in distilled water, 24.33 + 4.19 seconds in artificial gastric fluid and 21.33 + 2.87 seconds in artificial intestine fluid. After a freeze-thaw test there was no change on the emulsion’s clarity, color, smell, as well as no separation, which means that the formula was stable thermodynamically. The optimum SNEDDS formula resulted has small particle size, better emulsifying time in artificial gastric and intestine fluids, as well as better thermodynamic stability, which in turn will improve the cytotoxic activity of the Curcuma mangga Val. rhizome oil toward cancer cells.

scholarly journals Formulation, in-vitro and in-vivo pharmacokinetic evaluation of simvastatin nanostructured lipid carrier loaded transdermal drug delivery system

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
S Brito Raj ◽  
Kothapalli Bonnoth Chandrasekhar ◽  
Kesavan Bhaskar Reddy
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Dosage ◽  
Pharmacokinetic Studies ◽  
Nanostructured Lipid Carrier ◽  
Transdermal Patch

Abstract Background A simvastatin nanostructured lipid carrier loaded transdermal patch was developed to enhance the bioavailability and therapeutic effect. Methods Simvastatin NLC preparation was prepared by optimized hot homogenization technique and were characterized by particle size in nanometer, polydispersity index, zeta potential in millivolt, scanning electron microscopy, and entrapment efficiency by applying Box Behnken design utilizing multiple linear regression method. Results Chosen optimized NLC F7 formulation has particle size of 125.4 ± 2.66 nm, zeta potential of − 33.6 ± 2.42 mV, and PI of 0.480 ± 0.24. The NLC was loaded in transdermal patch by solvent evaporation method and evaluated for physical characteristics, drug content, skin permeation studies, and in-vivo pharmacokinetic studies in male albino Wistar rat. In-vivo pharmacokinetic studies in NLC loaded transdermal patch show an increase in AUC0-α in mg/ml when compared to marketed oral dosage form, which confirms the enhancement of bioavailability of simvastatin by NLC loaded transdermal patch. Conclusions From the data, it was concluded that drug-loaded NLC transdermal patch will be a promising drug delivery system for poorly bioavailable drugs.

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